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4-苄氧基-1-硝基苯置于盐酸,Tin(II) Chloride Dihdyrate体系中,用 乙醇 作为反应溶剂,化学反应 9.0H,以91%的收率获得产物4-苯甲氧基苯胺盐酸盐
参考文献:四氢咔唑衍生物作为潜在降糖药的设计,合成和评价
标题:四氢咔唑衍生物作为潜在降糖药的设计,合成和评价
摘要:基于 Zg02 设计和合成了两个系列的四氢咔唑衍生物,Zg02 是我们之前研究中开发的有前景的候选物.在 Hepg2 细胞系中筛选新制备的化合物的葡萄糖消耗活性.氮杂-四氢咔唑化合物12B显示出最有效的降血糖活性,与溶剂对照相比,葡萄糖消耗增加了 45%,其活性比阳性对照化合物(二甲双胍和 Zg02)高约 1.2 倍.对潜在机制的研究表明,12B可能通过激活 Ampk 途径表现出降血糖活性.代谢稳定性分析表明,12B在来自 Sd 大鼠的人造胃肠液和血浆中均显示出非常好的稳定性.进行了口服葡萄糖耐量试验 (Ogtt),结果进一步证实12B是一种有效的降血糖药.
DOI:10.1016/j.Bioorg.2021.105172

专利信息

专利号:US-10844047-B2
优先权日:2018-06-21
标题:Process for the preparation of bazedoxifene
发明人：FERRARI MASSIMO; ZANI DANIELE DE; VEZZOSI STEFANO; BELOTTI PAOLO
权利人:ERREGIERRE SPA
摘要:The invention relates to a process for preparation of the compound 3-methyl-5-benzyloxy-2-(4-benzyloxyphenyl)-1H-indole 5, an intermediate for the synthesis of bazedoxifene and bazedoxifene acetate.

专利号:US-6916949-B2
优先权日:2001-01-29
标 题 :Methods of chemical systhesis of phenolic nitrogen mustard prodrugs
发明人：SPRINGER CAROLINE JOY; NICULESCU-DUVAZ DAN
权利人:CANCER REC TECH LTD
摘要:This invention pertains to novel methods for the synthesis of certain nitrogen mustard prodrugs, such as N-{4-[N,N-bis(2-haloethylamino)-phenoxycarbonyl}-L-glutamic acid: wherein: X² is a halo group, and is -F, -Cl, -Br, or -I; n is an integer from 0 to 4; and, each R^A is an aryl substituent. The methods comprise, at least, the steps of: glutamate conjugation (GC); silyloxy deprotection (SD); and, sulfonic esterification (SU). Certain preferred methods comprise the steps of: amine substitution (AS); silyloxy protection (SP); phenolic deprotection (PD); activation (AC); glutamate conjugation (GC); silyloxy deprotection (SD); sulfonic estenfication (SU); halogenation (HL); glutamate deprotection (GD); and glutamic acid protection (GP).

专利号:WO-02060862-A1
优先权日:2001-01-29
标题:Methods of chemical synthesis of phenolic nitrogen mustard prodrugs

专利号:CN-116997544-A
优先权日:2021-03-24
标 题:Used in the synthesis of 5-{5-chloro-2-[(3S)-3-[(morpholin-4-yl)methyl]-3,4-dihydroisoquinoline-2(1H)-carbonyl]benzene New method of 1,2-dimethyl-1H-pyrrole-3-carboxylic acid derivatives and their application in the production of pharmaceutical compounds

专利号:EP-1355876-B1
优先权日:2001-01-29
标题:Methods of chemical synthesis of phenolic nitrogen mustard prodrugs

专利号:EP-1355876-A1
优先权日:2001-01-29
标题 :Methods of chemical synthesis of phenolic nitrogen mustard prodrugs